发明名称 |
Verfahren zur Herstellung von hetero-bizyklischem Alkohol-Enantiomer |
摘要 |
<p>The invention relates to a method for the stereoselective preparation of a hetero-bicyclic alcohol enantiomer, characterized in that a substantially pure enantiomer of the general formula <CHEM> wherein X is O, S, NH or N-(C1-C4)alkyl; Y1 and Y2 are each independently hydrogen or substituents selected from halogen, (C1-C4)alkyl, (C1-C4)alkoxy, (C1-C4)haloalkyl, formyl, nitro and cyano; the C*-atom has either the R or the S configuration; is prepared from a compound of the general formula <CHEM> wherein R1 is hydrogen or a suitable protective group and R2 is hydrogen or wherein R1 and R2 together form an optionally mono- or di-(C1-C3)alkyl substituted methylene bridge; by the following successive reaction steps: (i) reaction with a compound of the general formula <CHEM> wherein Z is a hydroxy group or a suitable leaving group, R3 is a hydroxy-protective group and R4 is a halogen atom; or wherein R3 and R4 together constitute a valence bond or a biradical of the formula -C(R11)2-O-, wherein R11 is a straight or branched (C1-C4)alkyl group and wherein the C*-atom has either the R or the S configuration; (ii) subjection of the compound formed to a deprotection/ring-closure reaction; (iii) optionally deprotection of the hydroxy group of the ring-closed product. The invention further relates to enantiomerically pure intermediates, the preparation of these intermediates and the preparation of a starting compound.</p> |
申请公布号 |
DE69714875(D1) |
申请公布日期 |
2002.10.02 |
申请号 |
DE1997614875 |
申请日期 |
1997.01.23 |
申请人 |
DUPHAR INTERNATIONAL RESEARCH B.V., WEESP |
发明人 |
BUIZER, NICOLAAS;KRUSE, CHRIS G.;SCHENK, KLARA M.;SHADID, BELAL |
分类号 |
C07D317/48;C07C205/22;C07C205/26;C07C205/37;C07C205/43;C07C217/84;C07D265/00;C07D265/36;C07D279/16;C07D303/20;C07D317/62;C07D319/20;C07D327/06;(IPC1-7):C07D319/20 |
主分类号 |
C07D317/48 |
代理机构 |
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代理人 |
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主权项 |
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地址 |
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